A1 Refereed original research article in a scientific journal

In-Vivo Bone-Targeting of Bis(phosphonate)-Conjugated Double Helical RNA Monitored by Positron Emission Tomography




AuthorsSatish Jadhav, Meeri Käkelä, Matthieu Bourgery, Kiira Rimpilä, Heidi Liljenbäck, Riikka Siitonen, Jussi Mäkilä, Tiina Laitala-Leinonen, Päivi Poijärvi-Virta, Harri Lönnberg, Anne Roivainen, Pasi Virta

PublisherAMER CHEMICAL SOC

Publication year2016

JournalMolecular Pharmaceutics

Journal name in sourceMOLECULAR PHARMACEUTICS

Journal acronymMOL PHARMACEUT

Volume13

Issue7

First page 2588

Last page2595

Number of pages8

ISSN1543-8384

DOIhttps://doi.org/10.1021/acs.molpharmaceut.6b00261(external)


Abstract
A bis(phosphonate) conjugate of 2'-O-methyl oligoribonucleotide (microRNA-21) was synthesized and used as a bone-targeting carrier in the systemic delivery of a Ga-68-1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA)chelated 2'-O-methyl oligoribonucleotide (anti-microRNA-21). The whole-body biodistribution of the double helical RNA was monitored by positron emission tomography (PET), which verified the expected bis(phosphonate)-induced bone accumulation in healthy rats.



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